摘要
以顺式或反式 - [2 -溴甲基 - 2 - (2 ,4 -二氯苯基 ) - 1,3-二氧戊环 - 4 -基 ]甲醇苯甲酸酯为原料 ,经与三唑缩合、水解、柱色谱纯化、甲磺酰化 ,最后与 4 - [4 - [4 - (4 -羟基苯基 ) - 1-哌嗪基 ]苯基 ]- 2 ,4 -二氢 - 2 - (1-甲基丙基 ) - 3H - 1,2 ,4 -三唑 -3-酮缩合 ,可分别得到抗真菌药物伊曲康唑 (1)的区域异构体 2或几何异构体 3。比较 1、2和 3的 1 HNMR谱学特征。 2和 3可作为 1质量控制的对照物。
The regio-isomer(2) and the geometrical isomer (3) of antifungal drug, itraconazole (1) were synthesized from cis- or trans-[2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methyl benzoate (4a or 4b) via condensation with triazole, hydrolysis, chromatographic purification, mesylation and condensation with 4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]-phenyl]-2,4-dihydro-2-(1-methyl- propyl)-3H-1,2,4-triazol-3-one. The 1HNMR data were compared among 1,2 and 3. Compounds 2 and 3 may be served as the references in the quality control of 1.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2003年第10期481-483,共3页
Chinese Journal of Pharmaceuticals
